Synthesis of Indomorphan Pseudo Natural Product Inhibitors of Glucose Transporters GLUT-1 and -3

Ceballos J, Schwalfenberg M, Karageorgis G, Reckzeh ES, Sievers S, Ostermann C, Pahl A, Sellstedt M, Nowacki J, Carnero Corrales M, Wilke J, Laraia L, Tschapalda K, Metz M, Sehr DA, Brand S, Winklhofer K, Janning P, Ziegler S, Waldmann H (2019) Angew Chem Int Ed Engl

doi: 10.1002/anie.201909518.

The Waldmann lab describes the design, synthesis and biologiocal evaluation of a collection of indomorphan pseudo NPs that combine biosynthetically unrelated indole- and morphan-alkaloid fragments. 

The so developed Glupin potently inhibits glucose uptake by selectively targeting glucose transporter GLUT-1 and Glut-3. Glupin suppresses glycolysis, reduces the levels of glucose-derived metabolites and attenuates the growth of various cancer cell lines.

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